Analgesic composition



Patented Aug. 24,1954

UNITED STATES PATENT OFFICE 2,687,366 ANALGESIC COMPOSITION Joseph Seifter, Willow Grove, Pa., assignor, by mesne assignments, to American Home Products Corporation, New York, N. Y., a corporation of Delaware Ne Drawing. Application March 20, 1951, Serial No. 216,653

4 Claims. (Cl. 16765) This invention relates to an analgesic comlicylates; phenyl cinchoninic acid; and similar position and more particularly to an improved compounds having like physilogical action. analgesic composition of the non-narcotic type In the preferred embodiment of my invention, having relatively minor cerebral stimulating efthe salts of N-methyl-omega-phenyltertiaryfeet. 5 butyl amine are used and as a particular prefer- It has been shown in the past that several ence, the sulfate salt of the amine. vasoconstrictors of the pressor amine type have The composition may be u ed in y Su b ability of increasing the analgesic effect of form, such as powders, tablets or solutions, or in various non-narcotic analgesics of the anticombination with various well-known extenders, pyretic type, noting U. S. Pat. No 2,427,887. binders or other excipients. Moreover, the active However, it has been found that while composiin redi nt may b p n n various m x r tions of this nature are in fact highly useful for of analgesic compounds or with th ingretheir analgesic action, they exert a strong cere- Cl e Su h as sedatives aIltiSpaSmOdicsbral stimulating effect, producing anxiety, rest- In general. the ingredients of the p lessness and insomnia in the ati nt, 5 tion will be used in proportions within about the Therefore, it is an object of my invention to board range: potentiate the analgesic action of the nonnarcotic analgesics so that a minimal dosage will Non-narcotic analgesic 50-500 provide the desired analgesic effect, Pressor amine salt -30 It is a further object of my invention to po- 20 tentiate said analgesic action by means of a composition that will not substantially raise the blood pressure, increase the heart rate, raise the blood sugar, disturb the vision, produce anxiety, restlessness, insomnia or other symptoms 21 of cerebral stimulation.

and in the preferred embodiment of my invention the pressor amine salt will be used in about the range of 5-15 mg. However, varying doses have been found effective for different conditions and I do not limit my invention to the ranges specified above.

Listed below are several examples of formulahave b able to aficPmplish the F tions that have been tried and found effective: tioned ob ects by combining as essential ingredients of the composition an analgesic of the Emmple] non-narcotic type and the pressor amine N- methyl-omega-phenyl-tertiary-butyl amine or Acetylsahcyhc acld 325 nOmwXiC salts thereof N methyl omega phenyl tertiary butyl In such a combination, it has been found that amme su1fate 5 the addition of moderate amounts of pressor Example II amine to a normal dosage of the analgesic Mg. synergistically potentiates the pain relieving Acetylsalicylic acid 195 power of the analgesic to an extent that would Phenacetin 195 not be expected from a knowledge of the proper- N methyl omega phenyl tertiary butyl ties of the two substances. Moreover, the inamine sulfate 10 creased analgesic effect is not accompanied by Example In any substantal symptoms of central cerebral stimulation, nor on the other hand does the pres- Acetanmd 300 sor amine potentiate the general depressing N methy] omega, phenyl tertiary butyl action of the benzenoid analges1cs. Therefore,

amine sulfate 5 such a combination provides the desired relief from pain with no untoward effects of stimula- Example IV tion or depression, enabling use of the analgesic composition of this invention before retiring or Phenacetm 300 the administration of massive doses large enough N methyl omega phenyl ternary butyl to prevent severe pain without undue stimulaamme Sulfate 5 tion or depression during the day. Example V As examples of the analgesics contemplated Mg. by the invention are the non-narcotic analgesics Salicylamid 50 of the benzene series such as acetylsalicylic acid, N methyl omega phenyl tertiary butyl acetanilid, phenacetin, salicylamid, and the saamine sulfate I claim:

'1. An analgesic comprising, in combination, acetylsalicylic acid and a non-toxic salt of N- methyl omega phenyl tertiary butyl amine wherein said non-toxic salt increases the analgesic effect of the analgesic while producing no substantial symptoms of central cerebral stimulation.

2. An analgesic composition comprising, in combination, the analgesic, acetylsalicylic acid, and a nontoxic salt of N-methyl-omega-phenyltertiary-butyl amine wherein said non-toxic salt increases the analgesic efiect of the analgesic while producing no substantial symptoms of central cerebral stimulation and in which the proportions of the non-toxic salt of N-methylomega-phenyl-tertiary-butyl amine and the analgesic are from about 25-30 mg. of the nontoxic salt with from about 50-500 mg. of the analgesic.

3. An analgesic composition comprising the analgesic, acetylsalicylic acid, and a non-toxic salt of N-methyl-omegaphenyl-tertiary-butyl amine wherein said analgesic and the non-toxic salt are present in the proportions of about 325 mg. of the analgesic to 5-15 mg. of the non-toxic salt.

4. An analgesic composition comprising acetylsalicylic acid and N-methyl-omega-phenyltertiary-butyl amine sulfate.

References Cited in the file of this patent UNITED STATES PATENTS OTHER REFERENCES Weston et al., J. A. c. s., vol. 65, pages 674-676. Suter, Medicinal Chemistry, vol. 1, New York, John Wiley and Sons, 1951, pages 391-2. 

1. AN ANALGESIC COMPRISING, IN COMBINATION, ACETYLSALICYLIC ACID AND A NON-TOXIC SALT OF NMETHYL - OMEGA - PHENYL - TERTIARY - BUTYL AMINE WHEREIN SAID NON-TOXIC SALT INCREASE THE ANALGESIC EFFECT OF THE ANALGESIC WHILE PRODUCING NO SUBSTANTIAL SYMPTOMS OF CENTRAL CEREBRAL STIMULATION. 